產(chǎn)品描述: | 6-Iodopravadoline is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors. |
靶點: |
Cannabinoid Receptor;CannabinoidReceptor |
體內(nèi)研究: |
6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used[1]. 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box, compared with vehicle group. |
參考文獻(xiàn): |
1.Mukherjee, Sutapa., et al. Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors. European Journal of Pharmacology (2004), 505(1-3), 1-9. 2.Geng, D. C., et al. Inhibition of titanium particle-induced inflammatory osteolysis through inactivation of cannabinoid receptor 2 by AM630. Journal of Biomedical Materials Research, Part A (2010), 95A(1), 321-326. 3.Patil, Mayur., et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology (2011), 61(4), 778-788. 4.Garcia-Gutierrez, Maria S., et al. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABAA receptors. British Journal of Pharmacology (2012), 165(4), 951-964. 5.Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814. |
溶解性: |
DMSO:50 mg/mL (99.14 mM),Need ultrasonic |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.983 ml |
9.914 ml |
19.827 ml |
5 mM |
0.397 ml |
1.983 ml |
3.965 ml |
10 mM |
0.198 ml |
0.991 ml |
1.983 ml |
50 mM |
0.04 ml |
0.198 ml |
0.397 ml |
|
注意: |
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